Preparation of Paclitaxel Nanocrystals Coated with Folic Acid-Modified Phospholipids Based on Preoperative Chemotherapy for Gastric Cancer

Abstract

This paper aims to develop a folate-modified phospholipid-coated paclitaxel nanocrystal (PTX NC@FA) for preoperative local chemotherapy of gastric cancer. PTX NC@FA was prepared by “small to large” method followed by ultrasonic method, and its particle morphology, particle size distribution, zeta-potential, drug content, folic acid-modified phospholipid (FA-DSPE-PEG2000) content, crystal characteristics and stability were investigated. The results showed that PTX NC@FA was short rod-shaped ans is stable in phosphate buffer or serum-containing phosphate buffer for at least 4 days, and can release drug slowly within 96 h. After a single peritumor injection, PTX NC@FA had significantly better tumor-inhibiting effect than non-folic acid-modified nanocrystals and commercial paclitaxel injection. After 12 days of administration to nude mice, the tumors in the PTX NC@FA group completely disappeared, and the tumor inhibition rate was 100%. The results suggest that PTX NC@FA has good application potential and is expected to be used to shrink tumors before surgery, increase the chance of gastric preservation, and improve the quality of life of patients after surgery.